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Assay Detail

CHEMBL807969

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125 I]-Tyr8 SP from the cloned human Tachykinin receptor 1 expressed in CHO cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Substance-P receptor (CHEMBL249)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.
Ladduwahetty T, Baker R, Cascieri MA, Chambers MS, Haworth K, Keown LE, MacIntyre DE, Metzger JM, Owen S, Rycroft W, Sadowski S, Seward EM, Shepheard SL, Swain CJ, Tattersall FD, Watt AP, Williamson DW, Hargreaves RJ.
J Med Chem (1996) 39 : 2907 -2914
PubMed 8709125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.95 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99055 1 10.30
CHEMBL99792 1 9.66
CHEMBL441225 CP-99994 1 9.30
CHEMBL95626 1 9.28
CHEMBL98811 1 9.10
CHEMBL101763 1 9.05
CHEMBL98022 1 9.01
CHEMBL99873 1 9.00
CHEMBL27003 1 8.89
CHEMBL100141 1 7.44
CHEMBL327736 1 7.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99055 IC50 = 0.05 nM 10.30
CHEMBL99792 IC50 = 0.22 nM 9.66
CHEMBL441225 CP-99994 IC50 = 0.5 nM 9.30
CHEMBL95626 IC50 = 0.53 nM 9.28
CHEMBL98811 IC50 = 0.8 nM 9.10
CHEMBL101763 IC50 = 0.9 nM 9.05
CHEMBL98022 IC50 = 0.97 nM 9.01
CHEMBL99873 IC50 = 1.0 nM 9.00
CHEMBL27003 IC50 = 1.3 nM 8.89
CHEMBL100141 IC50 = 36.0 nM 7.44
CHEMBL327736 IC50 = 43.0 nM 7.37